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122 条记录 (耗时 0.043 秒)

    CYCLIC TRIAZO AND DIAZO SODIUM CHANNEL BLOCKERS
    29.
    发明申请
    CYCLIC TRIAZO AND DIAZO SODIUM CHANNEL BLOCKERS 有权
    环状三唑和二氧化硅通道阻塞剂

    公开(公告)号：US20110009413A1

    公开(公告)日：2011-01-13

    申请号：US12811884

    申请日：2009-01-16

    申请人： Michael Leach ,  Laurence Harbige ,  Dieter Riddall ,  Karl Franzmann

    发明人： Michael Leach ,  Laurence Harbige ,  Dieter Riddall ,  Karl Franzmann

    IPC分类号： A61K31/53 ,  C07D253/075 ,  C07D405/04 ,  C07D403/12 ,  C07D409/04 ,  C07D253/07 ,  C07D405/14 ,  C07D401/04 ,  A61P25/08 ,  A61P25/00 ,  A61P27/06 ,  A61P25/28 ,  A61P25/16 ,  A61P25/06 ,  A61P25/18 ,  A61P25/22 ,  A61P29/00

    CPC分类号： C07D253/075 ,  C07D253/06 ,  C07D253/07 ,  C07D253/10 ,  C07D401/04 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12

    摘要： Compounds of general structure in which X and Y are each N or C with at least one of X and Y being N; Z is a single bond or an optionally substituted linking group R1 is hydrogen or a substituent group; R2 is amino or a substituent group; N* is amino when RI is hydrogen or ═NH when R1 is a substituent group; or N* is a group NRaRb where Ra and Rb are independently H or an alkyl group; or N* is an optionally substituted piperazinyl ring; and A is an optionally substituted heterocyclic or carbocyclic ring system which may be linked to the triazo/diazo ring through R2 to form a fused multicyclic ring; are indicated as suitable for treatment of disorders in mammals that are susceptible to sodium channel blockers and antifolates, and particularly disorders such epilepsy, multiple sclerosis, glaucoma and uevitis, cerebral traumas and cerebral ischaemias, stroke, head injury, spinal cord injury, surgical trauma, neurodegenerative disorders, motorneurone disease, Alzheimer's disease, Parkinson's disease, chronic inflammatory pain, neuropathic pain, migraine, bipolar disorder, mood, anxiety and cognitive disorders, schizophrenia and trigeminal autonomic cephalalgias; for treatment of mammalian cancers; and for treatment of malaria.

    摘要翻译： X和Y各自为N或C，X和Y中的至少一个为N的一般结构化合物; Z是单键或任选取代的连接基团R 1是氢或取代基; R2是氨基或取代基; 当R 1为氢时，N *为氨基，或当R 1为取代基时为= NH; 或N *为NRaRb基团，其中Ra和Rb独立地为H或烷基; 或N *是任选取代的哌嗪基环; 并且A是任选取代的杂环或碳环系，其可以通过R 2与三偶氮/重氮环连接以形成稠合多环; 适用于治疗对钠通道阻滞剂和抗叶酸剂敏感的哺乳动物的疾病，特别是诸如癫痫，多发性硬化，青光眼和uev病，脑创伤和脑缺血性脑卒中，脑损伤，脊髓损伤，手术创伤 神经退行性疾病，运动​​神经元疾病，阿尔茨海默病，帕金森病，慢性炎性疼痛，神经性疼痛，偏头痛，双相情感障碍，情绪，焦虑和认知障碍，精神分裂症和三叉神经性自主性头痛。 用于治疗哺乳动物癌症; 并用于治疗疟疾。

    1,2,4-benzotriazine-1,4-dioxides
    30.
    发明授权
    1,2,4-benzotriazine-1,4-dioxides 有权
    1,2,4-苯并三嗪-1,4-二氧化物

    公开(公告)号：US07816521B2

    公开(公告)日：2010-10-19

    申请号：US10590796

    申请日：2005-03-01

    申请人： William Alexander Denny ,  Michael Patrick Hay ,  Kevin Owen Hicks ,  Frederik Pruijn ,  William Robert Wilson ,  Karin Pchalek

    发明人： William Alexander Denny ,  Michael Patrick Hay ,  Kevin Owen Hicks ,  Frederik Pruijn ,  William Robert Wilson ,  Karin Pchalek

    IPC分类号： C07D253/10 ,  C07D413/12 ,  A61K31/53 ,  A61P35/00

    CPC分类号： C07D253/10 ,  C07D253/08 ,  C07D401/12

    摘要： The compound 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide and pharmacologically acceptable salts thereof. A method of treating cancer in a subject is also described in which 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide or a pharmacologically acceptable salt thereof is administered to tumor cells in a hypoxic environment. Also described is a method of radiosensitising in a subject tumor cells of solid tumors in hypoxic conditions by administering to the subject a pharmaceutical composition containing 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide or a pharmacologically acceptable salt thereof in an amount sufficient to produce radiosensitivity in the tumor cells, and subjecting the tumor cells to radiation. A pharmaceutical composition is additionally provided containing a therapeutically effective amount of 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide or a pharmacologically acceptable salt thereof and a pharmaceutically acceptable excipient, adjuvant, carrier, buffer or stabiliser.

    摘要翻译： 化合物3-乙基-6- [3-（4-吗啉基）丙氧基] -1,2,4-苯并三嗪1,4-二氧化物及其药理学上可接受的盐。 还描述了在受试者中治疗癌症的方法，其中给予3-乙基-6- [3-（4-吗啉基）丙氧基] -1,2,4-苯并三嗪1,4-二氧化物或其药理学上可接受的盐 到缺氧环境中的肿瘤细胞。 还描述了通过向受试者施用含有3-乙基-6- [3-（4-吗啉基）丙氧基] -1,2,4-恶二唑的药物组合物，在缺氧条件下的实体瘤的受试肿瘤细胞中放射增敏的方法， 苯并三嗪1,4-二氧化物或其药理学上可接受的盐，其量足以在肿瘤细胞中产生放射敏感性，并对肿瘤细胞进行辐射。 另外提供含有治疗有效量的3-乙基-6- [3-（4-吗啉基）丙氧基] -1,2,4-苯并三嗪1,4-二氧化物或其药学上可接受的盐和药学上可接受的盐的药物组合物 可接受的赋形剂，佐剂，载体，缓冲液或稳定剂。